Assay Detail
Binding
CHEMBL1013146
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]testosterone from human recombinant androgen receptor T877A mutant expressed in LNCaP cells
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | LNCaP |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
4-(Anilino)pyrrole-2-carboxamides: Novel non-steroidal/non-anilide type androgen antagonists effective upon human prostate tumor LNCaP cells with mutated nuclear androgen receptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 17 | 7.56 | 8.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL481139 | — | — | 1 | 8.52 |
| CHEMBL519112 | — | — | 1 | 8.52 |
| CHEMBL491 | HYDROXYFLUTAMIDE | 2.0 | 1 | 8.52 |
| CHEMBL518945 | — | — | 1 | 8.30 |
| CHEMBL480955 | — | — | 1 | 8.22 |
| CHEMBL480959 | — | — | 1 | 8.15 |
| CHEMBL503676 | — | — | 1 | 8.05 |
| CHEMBL63560 | (R)-BICALUTAMIDE | — | 1 | 8.00 |
| CHEMBL520428 | — | — | 1 | 7.57 |
| CHEMBL521249 | — | — | 1 | 7.44 |
| CHEMBL481924 | — | — | 1 | 7.31 |
| CHEMBL521251 | — | — | 1 | 7.00 |
| CHEMBL479988 | — | — | 1 | 6.89 |
| CHEMBL481939 | — | — | 1 | 6.89 |
| CHEMBL481107 | — | — | 1 | 6.85 |
| CHEMBL480934 | — | — | 1 | 6.48 |
| CHEMBL481746 | — | — | 1 | 5.85 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL481139 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL519112 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL491 | HYDROXYFLUTAMIDE | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL518945 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL480955 | — | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL480959 | — | Ki | = | 7.0 | nM | 8.15 |
| CHEMBL503676 | — | Ki | = | 9.0 | nM | 8.05 |
| CHEMBL63560 | (R)-BICALUTAMIDE | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL520428 | — | Ki | = | 27.0 | nM | 7.57 |
| CHEMBL521249 | — | Ki | = | 36.0 | nM | 7.44 |
| CHEMBL481924 | — | Ki | = | 49.0 | nM | 7.31 |
| CHEMBL521251 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL479988 | — | Ki | = | 130.0 | nM | 6.89 |
| CHEMBL481939 | — | Ki | = | 130.0 | nM | 6.89 |
| CHEMBL481107 | — | Ki | = | 140.0 | nM | 6.85 |
| CHEMBL480934 | — | Ki | = | 330.0 | nM | 6.48 |
| CHEMBL481746 | — | Ki | = | 1400.0 | nM | 5.85 |